• 产品描述： T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG

• 靶点： Hec1/Nek2;Apoptosis; MicrotubuleAssociated

• 体外研究：
  T-1101 tosylate shows potent in vitro antiproliferative activity (IC50: 14.8-21.5 nM). T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells. T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner. T-1101 tosylate (1 µM; 24 hours) induces apoptosis. T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1. Apoptosis Analysis Cell Line: HeLa cells Concentration: 1 µM Incubation Time: 24 hours Result: Increased the amount of apoptotic marker proteins cleaved caspase-3 and PARP and decreased the amount of antiapoptotic proteins Mcl-1 and XIAP in HeLa cells. Western Blot Analysis Cell Line: K562 cells Concentration: 1 μM Incubation Time: 3 hours, 6 hours, 16 hours, 24 hours Result: Lowered the level of Nek2 in a time-dependent manner.

• 体内研究：
  T-1101 tosylate shows good oral bioavailability and thermal stability. Oral co-administration of T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) halves the dose of sorafenib (25 mg/kg to 12.5 mg/kg) required to exhibit comparable in vivo activity towards Huh-7 xenografts. T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts. Animal Model: SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts Dosage: 25 mg/kg, 50 mg/kg Administration: Oral administration; twice per day; 28 days Result: Showed significant in vivo activity in mice bearing various human cancer xenografts.

• 参考文献：
  1. Chuang SH, et al. Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Eur J Med Chem. 2020 Apr 1;191:112118.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.502 ml	7.51 ml	15.02 ml
  5 mM	0.3 ml	1.502 ml	3.004 ml
  10 mM	0.15 ml	0.751 ml	1.502 ml
  50 mM	0.03 ml	0.15 ml	0.3 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *